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| Targets |
Beinaglutide targets the glucagon-like peptide-1 receptor (GLP-1R), a G protein-coupled receptor expressed primarily on pancreatic beta cells, as well as on the brain, heart, and gastrointestinal tract. As a GLP-1 receptor agonist, Beinaglutide binds to GLP-1R and activates downstream signaling pathways, including the cAMP/PKA pathway. This activation leads to glucose-dependent insulin secretion, suppression of glucagon release, delayed gastric emptying, and increased satiety. These effects collectively contribute to glycemic control and weight loss.
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| ln Vitro |
In adipocytes induced by increased insulin, benaglutide (100 nM; 48 hours) increases the expression of Akt phosphorylation [2].
In vitro, Beinaglutide acts as a potent GLP-1 receptor agonist. In cell-based assays using GLP-1R-expressing cells, Beinaglutide stimulates cAMP production, confirming its activity as a GLP-1 agonist. It enhances glucose-stimulated insulin secretion from pancreatic beta cells. The high homology with human GLP-1 ensures that it is recognized by the human GLP-1 receptor with high affinity. The peptide is used in cell culture studies to investigate the cellular mechanisms of GLP-1 signaling and its effects on insulin secretion and cellular metabolism. |
| ln Vivo |
In mice, beenaglutide (0.6, 1.2, 2.4 mg/kg; sc; three times daily for seven days) has been demonstrated to lower body weight, suppress food intake, and regulate blood sugar [1]. Adipocytes are more sensitive to insulin when benaglutide (150 μg/kg; sc; once daily for 6 weeks) is administered [2].
In vivo, Beinaglutide demonstrates dose-dependent effects in glycemic control, inhibition of food intake, gastric emptying, and promotion of weight loss. In mouse models, subcutaneous injection of Beinaglutide (0.6, 1.2, 2.4 mg/kg, three times daily for 7 days) showed significant blood glucose control, reduced food intake, and weight loss. It has the potential for the research of overweight/obesity and nonalcoholic steatohepatitis (NASH). Beinaglutide is a promising candidate for treating metabolic disorders. |
| Enzyme Assay |
For in vitro binding assays, a standard protocol uses radioligand binding with [125I]-GLP-1. Membranes prepared from cells overexpressing the human GLP-1 receptor are incubated with [125I]-GLP-1 (0.1 nM) and varying concentrations of Beinaglutide (0.1 pM - 100 nM) in binding buffer (50 mM HEPES, pH 7.4, 5 mM MgCl2, 0.1% BSA) for 2 hours at room temperature. Bound and free radioligands are separated by rapid filtration through GF/B filters presoaked in 0.5% polyethylenimine. Radioactivity is measured by gamma counting. The Ki is calculated from competition curves. For functional assays, cells are treated with Beinaglutide (0.1 pM - 100 nM), and cAMP levels are measured by HTRF.
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: 3T3L-1 cells Tested Concentrations: 100 nM Incubation Duration: 48 h Experimental Results: Increased the phosphorylation of Akt in the adipocytes that were potentiated insulin-stimulated. For in vitro cell-based assays, INS-1 rat insulinoma cells or human GLP-1R-expressing HEK293 cells are seeded in 96-well plates. Cells are incubated in Krebs-Ringer bicarbonate buffer (KRB) with 0.1% BSA and 2.8 mM glucose for 1 hour. They are then treated with varying concentrations of Beinaglutide (0.1-1000 nM) in the presence of 5-20 mM glucose for 1 hour. Supernatants are collected, and insulin concentration is measured by ELISA. To measure cAMP, cells are lysed after treatment, and cAMP levels are quantified using a competitive immunoassay. The EC50 for insulin secretion or cAMP production is calculated. |
| Animal Protocol |
Animal/Disease Models: Wild-type male C57BL/6 mice and Male Lepob/Lepob (ob/ob) mice (ob/ob-NASH mouse model was induced by GAN diet)[1]
Doses: 0.6, 1.2, 2.4 mg/kg Route of Administration: Sc; three times per day for 7 days Experimental Results: Dramatically decreased blood glucose with dosedependence in C57BL/6 and ob/ob mice, dose dependently inhibits food intake and gastric Emptying, and Dramatically decreased body weight, food intake with dose-dependence . Animal/Disease Models: Eightweeks old male C57BL/6 mice[2] Doses: 150 µg/kg Route of Administration: Sc; daily for 6 weeks Experimental Results: demonstrated improved glucose tolerance and insulin sensitivity, diminished adipose tissue weight and adipocyte size and potentiated insulin sensitivity of adipocytes. For in vivo animal studies, a mouse model of obesity or diabetes is used (e.g., high-fat diet-induced obese mice or db/db mice). Beinaglutide is administered subcutaneously once daily at doses of 0.3-2.4 mg/kg for 4-8 weeks. Control animals receive vehicle (saline). Blood glucose is measured weekly using a glucometer. Food intake is measured daily. Body weight is recorded weekly. An oral glucose tolerance test (OGTT) is performed at week 4. At study endpoint, blood is collected for measurement of HbA1c and insulin levels, and pancreatic tissues are harvested for immunohistochemistry to assess beta cell mass. |
| ADME/Pharmacokinetics |
Beinaglutide, as a recombinant peptide, has a molecular weight of approximately 3298.61 Da. Due to its peptide nature, it has low oral bioavailability and is administered subcutaneously. In preclinical studies, Beinaglutide shows a half-life of approximately 1-2 hours in rodents, requiring multiple daily injections (three times daily for 7 days in mouse studies). The volume of distribution is similar to plasma volume, and clearance occurs via proteolytic degradation. For extended duration of action, the peptide can be formulated with sustained-release technologies or genetically modified for longer half-life.
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| Toxicity/Toxicokinetics |
Specific toxicology data for Beinaglutide is limited, as it is a research compound. As a GLP-1 receptor agonist, it is expected to have a safety profile similar to other GLP-1 drugs (e.g., exenatide, liraglutide). Common adverse effects include gastrointestinal symptoms such as nausea, vomiting, and diarrhea, which are typically dose-dependent and diminish with continued use. Potential long-term risks include pancreatitis and thyroid C-cell tumors, which have been observed in animal studies with some GLP-1 agonists. The compound is not intended for human use in a research setting and is for laboratory use only.
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| References |
[1]. Fang X, et al. Beinaglutide shows significantly beneficial effects in diabetes/obesity-induced nonalcoholic steatohepatitis in ob/ob mouse model. Life Sci. 2021 Apr 1;270:118966.
[2]. Zhang F, et al. Recombinant human GLP-1 beinaglutide regulates lipid metabolism of adipose tissues in diet-induced obese mice. iScience. 2021 Oct 30;24(12):103382. |
| Additional Infomation |
Benaglutide is currently being studied in the clinical trial NCT03829891 (Study on glycemic variability of benaglutide in combination with insulin glargine for the treatment of type 2 diabetes).
Beinaglutide is a recombinant human GLP-1 (rhGLP-1) polypeptide that shares almost 100% homology with human GLP-1 (7-36). It is also known as a novel recombinant human GLP-1 and is being investigated for its therapeutic potential in treating obesity and nonalcoholic steatohepatitis (NASH). Unlike synthetic GLP-1 analogs (e.g., exenatide, liraglutide), Beinaglutide is structurally identical to the endogenous human hormone, which may reduce immunogenicity. The compound is not approved for clinical use and is supplied for research purposes only. It is not a pharmaceutical drug and has no clinical approval status. |
| Molecular Formula |
C149H225N39O46
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|---|---|
| Molecular Weight |
3298.61453509331
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| Exact Mass |
3297.649
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| CAS # |
123475-27-4
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| PubChem CID |
131801470
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| Appearance |
White to off-white solid powder
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| LogP |
-13.6
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| Hydrogen Bond Donor Count |
49
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| Hydrogen Bond Acceptor Count |
51
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| Rotatable Bond Count |
109
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| Heavy Atom Count |
234
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| Complexity |
7660
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| Defined Atom Stereocenter Count |
30
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)O)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)N)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC5=CC=CC=C5)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC6=CNC=N6)N
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| InChi Key |
NGJOFQZEYQGZMB-KTKZVXAJSA-N
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| InChi Code |
InChI=1S/C149H225N39O46/c1-17-76(10)119(145(230)166-80(14)125(210)174-104(60-86-63-158-91-36-25-24-35-89(86)91)135(220)176-100(56-73(4)5)136(221)185-117(74(6)7)143(228)173-92(37-26-28-52-150)127(212)159-66-111(197)168-98(148(233)234)39-30-54-157-149(154)155)187-137(222)102(57-83-31-20-18-21-32-83)177-132(217)97(47-51-115(203)204)172-131(216)93(38-27-29-53-151)169-123(208)78(12)163-122(207)77(11)165-130(215)96(44-48-109(153)195)167-110(196)65-160-129(214)95(46-50-114(201)202)171-133(218)99(55-72(2)3)175-134(219)101(59-85-40-42-88(194)43-41-85)178-140(225)106(68-189)181-142(227)108(70-191)182-144(229)118(75(8)9)186-139(224)105(62-116(205)206)179-141(226)107(69-190)183-147(232)121(82(16)193)188-138(223)103(58-84-33-22-19-23-34-84)180-146(231)120(81(15)192)184-112(198)67-161-128(213)94(45-49-113(199)200)170-124(209)79(13)164-126(211)90(152)61-87-64-156-71-162-87/h18-25,31-36,40-43,63-64,71-82,90,92-108,117-121,158,189-194H,17,26-30,37-39,44-62,65-70,150-152H2,1-16H3,(H2,153,195)(H,156,162)(H,159,212)(H,160,214)(H,161,213)(H,163,207)(H,164,211)(H,165,215)(H,166,230)(H,167,196)(H,168,197)(H,169,208)(H,170,209)(H,171,218)(H,172,216)(H,173,228)(H,174,210)(H,175,219)(H,176,220)(H,177,217)(H,178,225)(H,179,226)(H,180,231)(H,181,227)(H,182,229)(H,183,232)(H,184,198)(H,185,221)(H,186,224)(H,187,222)(H,188,223)(H,199,200)(H,201,202)(H,203,204)(H,205,206)(H,233,234)(H4,154,155,157)/t76-,77-,78-,79-,80-,81+,82+,90-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,117-,118-,119-,120-,121-/m0/s1
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| Chemical Name |
(4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]propanoyl]amino]-5-oxopentanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~1.79 mg/mL (~0.54 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3032 mL | 1.5158 mL | 3.0316 mL | |
| 5 mM | 0.0606 mL | 0.3032 mL | 0.6063 mL | |
| 10 mM | 0.0303 mL | 0.1516 mL | 0.3032 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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